Boiwe T, Bränden C I
Eur J Biochem. 1977 Jul 1;77(1):173-9. doi: 10.1111/j.1432-1033.1977.tb11655.x.
We have studied the binding of two inhibitor molecules, imidazole and 1,10-phenanthroline, to liver alcohol dehydrogenase by crystallographic methods. X-ray data for the imidazole complex were collected to 0.29-nm resolution and for the 1,10-phenanthroline complex to 0.45-nm resolution. In both cases we found only one peak in the difference electron density maps close to the active zinc atom. The peak corresponding to 1,10-phenanthroline overlaps the site of the density of the zinc-bound water in the apoenzyme and the imidazole density partly overlaps this density. We can not discern any additional peaks close to the zinc atom which would correspond to new positions of bound water. We thus conclude that both these inhibitors bind to the catalytic zinc atom and that upon binding they displace the water molecule that is firmly bound to this zinc atom in the apoenzyme. We do not see any structural changes in the remaining part of the molecule.
我们通过晶体学方法研究了两种抑制剂分子,即咪唑和1,10-菲咯啉与肝脏乙醇脱氢酶的结合情况。收集了咪唑复合物的X射线数据,分辨率达到0.29纳米,1,10-菲咯啉复合物的数据分辨率为0.45纳米。在这两种情况下,我们在靠近活性锌原子的差分电子密度图中仅发现一个峰。对应于1,10-菲咯啉的峰与脱辅基酶中锌结合水的密度位点重叠,咪唑的密度部分与该密度重叠。我们在靠近锌原子处未发现任何对应于结合水新位置的额外峰。因此,我们得出结论,这两种抑制剂均与催化锌原子结合,并且结合时它们取代了脱辅基酶中牢固结合于该锌原子的水分子。我们未观察到分子其余部分有任何结构变化。